NAV

Alpha-1-proteinase inhibitor

Identification

Summary

Alpha-1-proteinase inhibitor is a purified form of human alpha-1 proteinase inhibitor used to treat emphysema patients with associated alpha-1 proteinase inhibitor deficiency.

Brand Names
Aralast, Glassia, Prolastin, Prolastin-C, Respreeza, Zemaira
Generic Name
Alpha-1-proteinase inhibitor
DrugBank Accession Number
DB00058
Background

Human alpha-1 proteinase inhibitor or alpha-1-antitrypsin, prepared from human plasma via Cohn alcohol fractionation followed by PEG and zinc chloride fractionation.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Protein Chemical Formula
C2001H3130N514O601S10
Protein Average Weight
44324.5 Da
Sequences
>DB00058 sequence
EDPQGDAAQKTDTSHHDQDHPTFNKITPNLAEFAFSLYRQLAHQSNSTNIFFSPVSIATA
FAMLSLGTKADTHDEILEGLNFNLTEIPEAQIHEGFQELLRTLNQPDSQLQLTTGNGLFL
SEGLKLVDKFLEDVKKLYHSEAFTVNFGDTEEAKKQINDYVEKGTQGKIVDLVKELDRDT
VFALVNYIFFKGKWERPFEVKDTEEEDFHVDQVTTVKVPMMKRLGMFNIQHCKKLSSWVL
LMKYLGNATAIFFLPDEGKLQHLENELTHDIITKFLENEDRRSASLHLPKLSITGTYDLK
SVLGQLGITKVFSNGADLSGVTEEAPLKLSKAVHKAVLTIDEKGTEAAGAMFLEAIPMSI
PPEVKFNKPFVFLMIEQNTKSPLFMGKVVNPTQK
Download FASTA Format
Synonyms
  • .Alpha.-1 protease inhibitor
  • .Alpha.1-proteinase inhibitor human
  • 122320-05-2
  • Alfa 1-proteinase inhibitor (human)
  • Alfa-1-antitripsina
  • Alfa1 antitrypsin
  • Alpha 1-antitrypsin
  • Alpha 1-Proteinase Inhibitor
  • Alpha 1-proteinase inhibitor (human)
  • Alpha 1-proteinase inhibitor human
  • Alpha 1-proteinase inhibitor, human
  • Alpha-1 protease inhibitor
  • Alpha-1 proteinase inhibitor (human)
  • Alpha-1-antiproteinase
  • Alpha-1-antitrypsin
  • Alpha-1-proteinase Inhibitor (human)
  • Alpha-1-proteinase inhibitor human
  • Alpha-1-proteinase Inhibitor, Human
  • Alpha-1-proteinase inhibitor,human
  • Alpha1-proteinase Inhibitor
  • Alpha1-proteinase inhibitor (human)
  • Alpha1-proteinase inhibitor human
  • Antileukoproteinase
  • API
  • Mucus proteinase inhibitor
  • Protease inhibitor wap4
  • Recombinant secretory leucocyte protease inhibitor
  • Recombinant secretory leukocyte protease inhibitor
  • Secretory leukocyte protease inhibitor (human)
  • SLPI
  • Wap four-disulfide core domain protein 4
External IDs
  • 232-924-7
  • ALP
  • HUSI-1
  • SLPI
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Pharmacology

Indication

For chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of emphysema.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofEmphysema•••••••••••••••••
Management ofEmphysema•••••••••••••••••
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Prevents excessive accumulation of active neutrophil elastase and consequent proteolysis of elastin tissues in alveolar lung structures. This prevents the development of emphysema.

Mechanism of action

Alpha-1 proteinase inhibitor is a serine protease inhibitor (Serpin). Its primary mechanism is inhibiting the action of the serine protease called elastase (also plasmin and thrombin) in the lungs. The reactive center loop (RCL) of alpha-1 proteinase inhibitor extends out from the body of the protein and directs binding to the target protease. The protease cleaves the serpin at the reactive site, establishing a covalent linkage between the carboxyl group of the serpin reactive site and the serine hydroxyl of the protease. The resulting inactive serpin-protease complex is highly stable.

TargetActionsOrganism
ANeutrophil elastase
inhibitor
Humans
Absorption

Not Available

Volume of distribution
  • 5632 ± 2006 mL [ARALAST NP]
  • 5618 ± 1618 mL [Aralast]
Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance
  • 940 +/- 275 mL/day [Patients with congenital α1-PI deficiency with single IV infusion of 60 mg/kg]
Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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interactions in your software
Albutrepenonacog alfaAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Albutrepenonacog alfa.
AlteplaseThe therapeutic efficacy of Alpha-1-proteinase inhibitor can be decreased when used in combination with Alteplase.
Aminocaproic acidAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Aminocaproic acid.
Andexanet alfaAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Andexanet alfa.
AnistreplaseThe therapeutic efficacy of Alpha-1-proteinase inhibitor can be decreased when used in combination with Anistreplase.
Food Interactions
No interactions found.

Products

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International/Other Brands
Aralast (Baxter) / Prolastin (Talecris Biotherapeutics C formerly Bayer)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Alpha1-proteinase Inhibitor (human)Powder, for solution1 g / vialIntravenousGrifols Therapeutics LlcNot applicableNot applicableCanada flag
Alpha1-proteinase Inhibitor (human)Powder, for solution500 mg / vialIntravenousGrifols Therapeutics LlcNot applicableNot applicableCanada flag
Aralast NPKit16 mg/1mLIntravenousBaxter Laboratories2010-04-192014-11-09US flag
Aralast NPInjection, powder, lyophilized, for solution; Kit16 mg/1mLIntravenousTakeda Pharmaceuticals America, Inc.2002-12-23Not applicableUS flag
Aralast NPKit16 mg/1mLIntravenousBaxter Laboratories2010-09-012014-11-09US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Prolastin-CAlpha-1-proteinase inhibitor (1000 mg/20mL) + Water (1 mL/1mL)Injection, powder, lyophilized, for solution; KitIntravenousGRIFOLS USA, LLC1987-12-02Not applicableUS flag

Categories

ATC Codes
B02AB02 — Alfa1 antitrypsin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
F43I396OIS
CAS number
9041-92-3

References

Synthesis Reference

Michael H. Coan, William J. Brockway, "Method of preparing alpha-1-proteinase inhibitor." U.S. Patent US4379087, issued December, 1968.

US4379087
General References
  1. Karnaukhova E, Ophir Y, Golding B: Recombinant human alpha-1 proteinase inhibitor: towards therapeutic use. Amino Acids. 2006 Jun;30(4):317-32. Epub 2006 May 26. [Article]
  2. FDA Approved Products: PROLASTIN® 5 -C LIQUID (Alpha1-Proteinase Inhibitor [Human]) Solution for Intravenous Injection [Link]
UniProt
P01009
Genbank
K01396
PubChem Substance
46506364
RxNav
535
Therapeutic Targets Database
DAP001102
PharmGKB
PA10308
RxList
RxList Drug Page
Wikipedia
Alpha-1_antitrypsin

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentPancreatitis, Chronic; Diabetes; Transplant1
4CompletedTreatmentAlpha 1-proteinase Inhibitor Deficiency / Emphysema2
4CompletedTreatmentAlpha-1 Anti-trypsin Deficiency1
4CompletedTreatmentAlpha-1 Anti-trypsin Deficiency / Healthy Subjects (HS)1
4RecruitingTreatmentBronchiectasis Adult1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Baxter International Inc.
  • CSL Behring LLC
  • Talecris Biotherapeutics
Dosage Forms
FormRouteStrength
Powder, for solutionIntravenous1 g / vial
Powder, for solutionIntravenous500 mg / vial
Injection, powder, lyophilized, for solution; kitIntravenous16 mg/1mL
KitIntravenous16 mg/1mL
Injection, solutionIntravenous1 g/50mL
SolutionIntravenous1000 mg / 50 mL
Injection, powder, for solutionParenteral1000 mg
Injection, powder, for solutionParenteral4000 mg
Injection, powder, for solutionParenteral5000 mg
InjectionIntravenous1000 mg
Powder, for solutionIntravenous25 mg / mL
Injection, powder, lyophilized, for solution; kitIntravenous
Injection; kitIntravenous1000 mg/20mL
Powder, for solutionIntravenous1000 mg / vial
Injection, solutionIntravenous1000 mg/20mL
SolutionIntravenous1000 mg / 20 mL
Injection, powder, lyophilized, for solutionIntravenous1000 mg
Injection, powder, for solutionIntravenous4000 mg
Injection, powder, for solutionIntravenous5000 mg
Powder, for solutionIntravenous1000 MG
Injection, powder, lyophilized, for solution; kitIntravenous1000 mg/20mL
Injection, powder, lyophilized, for solution; kitIntravenous4000 mg/76mL
Injection, powder, lyophilized, for solution; kitIntravenous5000 mg/95mL
Kit; powder, for solutionIntravenous1000 mg / vial
Kit; powder, for solutionIntravenous4000 mg / vial
Kit; powder, for solutionIntravenous5000 mg / vial
Injection, powder, for solutionIntravenous1000 mg
Prices
Unit descriptionCostUnit
Aralast 1000 mg vial0.52USD vial
Aralast np 1000 mg vial0.52USD vial
Aralast np 500 mg vial0.52USD vial
Aralast 500 mg vial0.5USD vial
Zemaira 1000 mg vial0.5USD vial
Prolastin 1000 mg vial0.46USD vial
Prolastin 500 mg vial0.46USD vial
Prolastin c 1000 mg vial0.46USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)59 °C at pH 7.8Tew D.J., Bottomley, S.P. J. Mol. Biol. 313:1161-1169 (2001)
hydrophobicity-0.302Not Available
isoelectric point5.37Not Available

Targets

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insights and accelerate drug research.
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Details1. Neutrophil elastase
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type endopeptidase activity
Specific Function
Modifies the functions of natural killer cells, monocytes and granulocytes. Inhibits C5a-dependent neutrophil enzyme release and chemotaxis.
Gene Name
ELANE
Uniprot ID
P08246
Uniprot Name
Neutrophil elastase
Molecular Weight
28517.81 Da
References
  1. Topic A, Ljujic M, Nikolic A, Petrovic-Stanojevic N, Dopudja-Pantic V, Mitic-Milikic M, Radojkovic D: Alpha-1-antitrypsin phenotypes and neutrophil elastase gene promoter polymorphisms in lung cancer. Pathol Oncol Res. 2011 Mar;17(1):75-80. doi: 10.1007/s12253-010-9283-5. Epub 2010 Jun 3. [Article]
  2. Karnaukhova E, Ophir Y, Golding B: Recombinant human alpha-1 proteinase inhibitor: towards therapeutic use. Amino Acids. 2006 Jun;30(4):317-32. Epub 2006 May 26. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55